Drug-Polymer Conjugates Coupled to a Peptidic Carrier
First Claim
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1. A monodisperse macromolecular conjugate composition for in-vivo delivery of a therapeutic agent comprising a peptidic carrier reversibly or irreversibly conjugated with:
- (a) one or more effectors and (b) one or more therapeutic agents, wherein said peptidic carrier comprises at least two different orthogonal pendant reactive groups each for specific attachment of a predetermined effector or therapeutic agent and at least one effector or therapeutic agent is attached to at least one of said pendant reactive groups on said peptidic carrier via a water-soluble polymer.
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Abstract
Monodisperse macromolecular conjugate compositions of a peptidic carrier irreversibly or reversibly conjugated with one or more effectors and one or more therapeutic agents, wherein at least one effector or therapeutic agent is attached to a pendant reactive group on said peptidic carrier via a water-soluble polymer. Monodispersity is obtained through the use of orthogonal and separate conjugation reactions.
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Citations
47 Claims
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1. A monodisperse macromolecular conjugate composition for in-vivo delivery of a therapeutic agent comprising a peptidic carrier reversibly or irreversibly conjugated with:
- (a) one or more effectors and (b) one or more therapeutic agents, wherein said peptidic carrier comprises at least two different orthogonal pendant reactive groups each for specific attachment of a predetermined effector or therapeutic agent and at least one effector or therapeutic agent is attached to at least one of said pendant reactive groups on said peptidic carrier via a water-soluble polymer.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 44, 45, 46, 47)
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41. A method for preparing a monodisperse macromolecular conjugate composition for in-vivo delivery of a therapeutic agent, wherein the macromolecular conjugate comprises a peptidic carrier conjugated with one or more effectors and one or more therapeutic agents, wherein the method comprises the steps of:
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(a) providing a peptidic carrier comprising first and second orthogonal pendant reactive groups, said first orthogonal pendant reactive group for specific attachment of a predetermined effector and said second orthogonal pendant reactive group for specific attachment of a predetermined therapeutic agent, wherein said peptidic carrier is selected from the group consisting of a peptide, a peptide mimetic, a pseudopeptide, and a peptide-related compound; (b) attaching said effector to said peptidic carrier by means of a water-soluble polymer such that each copy of an effector is attached to the same reactive groups on each peptidic carrier in the composition; and (c) attaching said therapeutic agent to said peptidic carrier by means of a water-soluble polymer such that each copy of a therapeutic agent is attached to the same reactive groups on each peptidic carrier in the composition.
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- 42. A monodisperse macromolecular conjugate composition comprising a peptidic carrier, wherein said peptidic carrier comprises at least two different orthogonal pendant reactive groups, wherein at least one of said pendant reactive groups on said peptidic carrier is attached to a water-soluble polymer.
Specification